名称 | Phenoxybenzamine hydrochloride |
描述 | Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen. |
细胞实验 | Phenoxybenzamine hydrochloride is dissolved in DMSO. After cytometry, 1×3 cells are implanted in a 96-well plate in 100 μL DMEM supplemented with 10 % FBS. Ten microliter (10 % of the total volume) WST-1 (Water Soluble Tetrazolium) is added to cells and incubated at 37°C for 30 min before colorimetric assay with 450 nm excitation and 630 nm emission at 24 h intervals up to 96 h. The mean fluorescence value is counted, and the cell number is determined using the standard curve. |
体外活性 | Phenoxybenzamine hydrochloride对[3H]yohimbine结合的阻断所导出的IC50(100 nM)明显低于其对Noradrenaline 引起的环磷酸腺苷(cyclic AMP)积累效应的逆转IC50(550 nM)[1]。Phenoxybenzamine hydrochloride(50 nM)与Phenoxybenzamine hydrochloridetolamine(1000 nM)联合使用比单独使用Phenoxybenzamine hydrochloride(50 nM)时更能增强Phenoxybenzamine hydrochlorideylephrine诱导的血管收缩,这一效果在完整内皮的主动脉中同样观察到。无论是dexmedetomidine(300或1000 nM)与Phenoxybenzamine hydrochloride(50 nM)的联合使用,还是Phenoxybenzamine hydrochloridetolamine(1000 nM)与Phenoxybenzamine hydrochloride(50 nM)的联合处理,相比单独使用Phenoxybenzamine hydrochloride(50 nM),都能增强Phenoxybenzamine hydrochlorideylephrine引发的收缩反应。此外,与dexmedetomidine(1000 nM)和Phenoxybenzamine hydrochloride的联合使用相比,Phenoxybenzamine hydrochloridetolamine与Phenoxybenzamine hydrochloride的联合使用在增强Phenoxybenzamine hydrochlorideylephrine引起的收缩方面更为显著。高浓度dexmedetomidine(1000 nM)与Phenoxybenzamine hydrochloride的联合使用,比低浓度dexmedetomidine(300 nM)与Phenoxybenzamine hydrochloride的联合使用,更能增强Phenoxybenzamine hydrochlorideylephrine诱发的收缩作用[2]。 |
体内活性 | Phenoxybenzamine hydrochloride(20 nM,皮下注射)有效抑制了小鼠中胶质瘤细胞的肿瘤生成,且Phenoxybenzamine hydrochloride-U87 mg移植瘤的细胞密度显著下降[3]。以Phenoxybenzamine hydrochloride(1 mg/kg,静脉注射)处理的大鼠在神经症状打分(NSS)和足失误评分方面显示出显著改善[4]。 |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | Ethanol : 63 mg/mL (185.1 mM) H2O : 14 mg/mL (41.1 mM) DMSO : 55 mg/mL (161.62 mM), Sonication is recommended.
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关键字 | Phenoxybenzamine hydrochloride | pheochromocytoma | Beta Receptor | neuroprotective | Phenoxybenzamine Hydrochloride | Inhibitor | Phenoxybenzamine | antitumor | NSC37448 | Adrenergic Receptor | hypertension | NSC-37448 | inhibit | glioma |
相关产品 | Buflomedil hydrochloride | Phenylephrine hydrochloride | Melatonin | Amitriptyline hydrochloride | Olanzapine | Trazodone hydrochloride | Mianserin hydrochloride | Gemfibrozil | Doxepin hydrochloride | Octopamine hydrochloride | Isoprenaline hydrochloride | Dexmedetomidine hydrochloride |
相关库 | 抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 抗癌上市药物库 | 已知活性化合物库 | 激酶抑制剂库 | GPCR靶点分子库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | FDA 上市激酶抑制剂库 |